Table 2. In Vitro Metabolic Stabilities and Permeability of Selected Compounds1.
| plasma
stability t1/2 (h), n = 3 |
human liver S9 stability t1/2 (min), n = 2 |
mouse liver S9 stability t1/2 (min), n = 2 |
|||||
|---|---|---|---|---|---|---|---|
| compound | human | mouse | phase I3 | phase II4 | phase I3 | phase II4 | PAMPA permeability Pe2 (10–6 cm/s), n = 6 |
| 3 | >245 | >245 | 674 ± 136 | >456 | 273 ± 23 | >456 | 0.2 ± 0.1 |
| 10 | >245 | >245 | 842 ± 210 | >456 | 28.9 ± 0.3 | >456 | 0.2 ± 0.1 |
| Verapamil | 19.2 ± 0.8 | 5.7 ± 0.1 | |||||
| Umbelliferone | 3.0 ± 0.05 | 0.8 ± 0.005 | |||||
1
Data are presented as mean ± SD.
2
Pe, Apparent permeability coefficient.
3
CYP enzyme cofactor: NADPH.
4
Cofactor: UDPGA.
5
No decrease in remaining percentage was observed at the end of incubation (24 h).
6
No decrease in remaining percentage was observed at the end of incubation (45 min).